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Synthesis and anti-HIV-1 activity of novel TSAO-T derivatives modified at the 2'- and 5'-positions of the sugar moiety.

Abstract：

:Novel analogues of the anti-HIV-1 agent TSAO-T, [1-[2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]thymine]-3'-spiro-5"-(4"-amino- 1",2"-oxathiole-2",2"-dioxide) and its 3-methyl counterpart TSAO-m3T were obtained by modifications at positions 2' or 5' of the sugar moiety. These compounds were evaluated for their inhibitory effect on HIV-1 and HIV-2 replication in cell culture. Introduction of new groups at the 5'-position (i.e. esters, benzylether and silylethers) resulted in compounds that were either inactive or less active than the parent compounds (TSAO-T and TSAO-m3T). Attempts to introduce small silyl ether groups at this position were not successful since these products decomposed during purification. Similar modifications at the 2'-position had a much less pronounced influence on the anti-HIV-1 activity.

journal_name

Antiviral Res

journal_title

Antiviral research

authors

Ingate S,Pérez-Pérez MJ,De Clercq E,Balzarini J,Camarasa MJ

doi

10.1016/0166-3542(95)00012-b

subject

Has Abstract

pub_date

1995-06-01 00:00:00

pages

281-99

issue

3

eissn

0166-3542

issn

1872-9096

pii

0166-3542(95)00012-B

journal_volume

27

pub_type

杂志文章

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